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EP2303269A4 - HAMMER OF ACT ACTIVITY - Google Patents

HAMMER OF ACT ACTIVITY

Info

Publication number
EP2303269A4
EP2303269A4 EP09759077A EP09759077A EP2303269A4 EP 2303269 A4 EP2303269 A4 EP 2303269A4 EP 09759077 A EP09759077 A EP 09759077A EP 09759077 A EP09759077 A EP 09759077A EP 2303269 A4 EP2303269 A4 EP 2303269A4
Authority
EP
European Patent Office
Prior art keywords
hammer
act activity
act
activity
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP09759077A
Other languages
German (de)
French (fr)
Other versions
EP2303269A1 (en
EP2303269B1 (en
Inventor
Hidetomo Furuyama
Yasuhiro Goto
Nobuhiko Kawanishi
Mark E Layton
Takashi Mita
Akira Naya
Yoshio Ogino
Yu Onozaki
Kevin J Rodzinak
Toshihiro Sakamoto
Philip E Sanderson
Jiabing Wang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
MSD KK
Merck Sharp and Dohme LLC
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of EP2303269A1 publication Critical patent/EP2303269A1/en
Publication of EP2303269A4 publication Critical patent/EP2303269A4/en
Application granted granted Critical
Publication of EP2303269B1 publication Critical patent/EP2303269B1/en
Not-in-force legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP09759077.2A 2008-06-03 2009-05-28 Inhibitors of akt activity Not-in-force EP2303269B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13075308P 2008-06-03 2008-06-03
PCT/US2009/045456 WO2009148916A1 (en) 2008-06-03 2009-05-28 Inhibitors of akt activity

Publications (3)

Publication Number Publication Date
EP2303269A1 EP2303269A1 (en) 2011-04-06
EP2303269A4 true EP2303269A4 (en) 2011-09-28
EP2303269B1 EP2303269B1 (en) 2014-07-30

Family

ID=41398446

Family Applications (1)

Application Number Title Priority Date Filing Date
EP09759077.2A Not-in-force EP2303269B1 (en) 2008-06-03 2009-05-28 Inhibitors of akt activity

Country Status (6)

Country Link
US (1) US8207169B2 (en)
EP (1) EP2303269B1 (en)
JP (1) JP2011522048A (en)
AU (1) AU2009255358A1 (en)
CA (1) CA2726317A1 (en)
WO (1) WO2009148916A1 (en)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011522048A (en) 2008-06-03 2011-07-28 メルク・シャープ・エンド・ドーム・コーポレイション Inhibitor of AKT activity
US8536193B2 (en) 2008-06-03 2013-09-17 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
WO2010104933A1 (en) * 2009-03-11 2010-09-16 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2405756B1 (en) 2009-03-12 2013-07-03 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY
GB0922589D0 (en) 2009-12-23 2010-02-10 Almac Discovery Ltd Pharmaceutical compounds
US20130102605A1 (en) * 2010-04-23 2013-04-25 Peng Liang Inhibitors of akt activity
JP5830094B2 (en) * 2010-07-12 2015-12-09 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ Substituted imidazo [1,2-a] pyrimidine and -pyridine
JP5926727B2 (en) 2010-07-28 2016-05-25 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ Substituted imidazo [1,2-b] pyridazine
PL2698372T3 (en) * 2011-04-06 2016-07-29 Taiho Pharmaceutical Co Ltd Novel imidazo-oxazine compound or salt thereof
CN103596957B (en) 2011-04-07 2016-12-07 拜耳知识产权有限责任公司 Imidazopyridazines as AKT kinase inhibitors
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
GB201205164D0 (en) 2012-03-23 2012-05-09 Almac Discovery Ltd Pharmaceutical compounds
ES2618003T3 (en) 2012-06-13 2017-06-20 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
KR20150034209A (en) 2012-06-26 2015-04-02 델 마 파마슈티컬스 인코포레이티드 Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
PL2868660T3 (en) * 2012-07-02 2018-05-30 Taiho Pharmaceutical Co., Ltd. Antitumor effect potentiator comprising an imidazooxazine compound
WO2014158644A1 (en) * 2013-03-13 2014-10-02 Dow Agrosciences Llc Process for the preparation of triaryl rhamnose carbamates
US20140275504A1 (en) * 2013-03-13 2014-09-18 Dow Agrosciences Llc Process for the preparation of certain triaryl rhamnose carbamates
AU2014251038A1 (en) 2013-04-08 2015-11-26 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
PT2986610T (en) 2013-04-19 2018-03-09 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US9231217B2 (en) * 2013-11-28 2016-01-05 Semiconductor Energy Laboratory Co., Ltd. Synthesis method of organometallic complex, synthesis method of pyrazine derivative, 5,6-diaryl-2-pyrazyl triflate, light-emitting element, light-emitting device, electronic device, and lighting device
WO2016113271A1 (en) * 2015-01-14 2016-07-21 Basf Se Imidazoisoquinoline compounds, compositions comprising the compounds and their use for controlling invertebrate pests
MA41551A (en) 2015-02-20 2017-12-26 Incyte Corp BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS
JPWO2016136928A1 (en) 2015-02-27 2017-08-31 大鵬薬品工業株式会社 IMIDAZOXOXAZINE CRYSTAL, PHARMACEUTICAL COMPOSITION CONTAINING THE CRYSTAL, AND METHOD FOR PRODUCING THE CRYSTAL
JP6853782B2 (en) * 2015-10-22 2021-03-31 田辺三菱製薬株式会社 New bicyclic heterocyclic compound
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
AR111960A1 (en) 2017-05-26 2019-09-04 Incyte Corp CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION
BR112020022392A2 (en) 2018-05-04 2021-02-02 Incyte Corporation solid forms of a fgfr inhibitor and processes for preparing them
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CN110092726B (en) * 2019-05-07 2022-04-08 山东省医学科学院药物研究所（山东省抗衰老研究中心、山东省新技术制药研究所） Synthesis method of Bictegravir intermediate
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
PH12022550892A1 (en) 2019-10-14 2023-05-03 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3162010A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
JP7720840B2 (en) * 2019-12-04 2025-08-08 インサイト・コーポレイション Tricyclic heterocycles as FGFR inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
JP2024522188A (en) 2021-06-09 2024-06-11 インサイト・コーポレイション Tricyclic Heterocycles as FGFR Inhibitors
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN119451960A (en) * 2022-08-05 2025-02-14 上海艾力斯医药科技股份有限公司 A condensed ring compound, preparation method and application thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008070016A2 (en) * 2006-12-06 2008-06-12 Merck & Co., Inc. Inhibitors of akt activity

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US6960584B2 (en) 2001-04-10 2005-11-01 Merck & Co., Inc. Inhibitors of Akt activity
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2002083138A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2003086403A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
EP1494675A4 (en) 2002-04-08 2006-07-19 Merck & Co Inc Inhibitors of akt activity
AU2003226271B2 (en) 2002-04-08 2007-10-18 Merck Sharp & Dohme Corp. Fused quinoxaline derivatives as inhibitors of Akt activity
EP1558586B1 (en) 2002-10-30 2011-03-30 Merck Sharp & Dohme Corp. Inhibitors of akt activity
CN1809354A (en) 2003-04-24 2006-07-26 麦克公司 Inhibitors of Akt activity
US7304063B2 (en) 2003-04-24 2007-12-04 Merck & Co., Inc. Inhibitors of Akt activity
US7638530B2 (en) 2003-04-24 2009-12-29 Merck & Co., Inc. Inhibitors of Akt activity
US7414055B2 (en) 2003-04-24 2008-08-19 Merck & Co., Inc. Inhibitors of Akt activity
CN1942470A (en) 2004-04-09 2007-04-04 默克公司 Inhibitors of AKT activity
JP2007532558A (en) 2004-04-09 2007-11-15 メルク　エンド　カムパニー　インコーポレーテッド Inhibitor of Akt activity
CN101217958A (en) 2004-08-23 2008-07-09 默克公司 Inhibitors of AKT activity
CA2588474A1 (en) 2004-12-02 2006-06-29 Merck & Co., Inc. Inhibitors of akt activity
AU2005316826A1 (en) 2004-12-15 2006-06-22 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
AU2006216998B2 (en) 2005-02-14 2010-12-23 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2602197A1 (en) 2005-04-12 2006-10-19 Merck & Co., Inc. Inhibitors of akt activity
NZ563423A (en) * 2005-06-10 2010-05-28 Merck Sharp & Dohme Inhibitors of AKT activity
WO2008070134A1 (en) 2006-12-06 2008-06-12 Merck & Co., Inc. Inhibitors of akt activity
JP2011522048A (en) 2008-06-03 2011-07-28 メルク・シャープ・エンド・ドーム・コーポレイション Inhibitor of AKT activity
US8536193B2 (en) 2008-06-03 2013-09-17 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
JP2012516847A (en) 2009-02-02 2012-07-26 メルク・シャープ・エンド・ドーム・コーポレイション Inhibitor of AKT activity
WO2010104933A1 (en) 2009-03-11 2010-09-16 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2405756B1 (en) 2009-03-12 2013-07-03 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008070016A2 (en) * 2006-12-06 2008-06-12 Merck & Co., Inc. Inhibitors of akt activity

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2009148916A1 *

Also Published As

Publication number Publication date
CA2726317A1 (en) 2009-12-10
US8207169B2 (en) 2012-06-26
EP2303269A1 (en) 2011-04-06
AU2009255358A1 (en) 2009-12-10
US20110092511A1 (en) 2011-04-21
JP2011522048A (en) 2011-07-28
EP2303269B1 (en) 2014-07-30
WO2009148916A1 (en) 2009-12-10

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